| Identification | Back Directory | [Name]
N-Ethyl-N'-[4-[5,6,7,8-tetrahydro-4-[(3S)-3-methyl-4-morpholinyl]-7-(3-oxetanyl)pyrido[3,4-d]pyrimidin-2-yl]phenyl]urea | [CAS]
1207360-89-1 | [Synonyms]
CS-695
RG-7603
GDC-0349
GDC-0349, RG7603
GDC-0349;GDC0349
GDC0349;GDC 0349;GDC 0349
(S)-1-Ethyl-3-(4-(4-(3-methylmorpholino)-7-(oxetan-3-yl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimi
(S)-1-ethyl-3-(4-(4-(3-methylmorpholino)-7-(oxetan-3-yl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-yl)phenyl)urea
N-Ethyl-N'-[4-[5,6,7,8-tetrahydro-4-[(3S)-3-methyl-4-morpholinyl]-7-(3-oxetanyl)pyrido[3,4-d]pyrimidin-2-yl]phenyl]urea
Urea, N-ethyl-N'-[4-[5,6,7,8-tetrahydro-4-[(3S)-3-methyl-4-morpholinyl]-7-(3-oxetanyl)pyrido[3,4-d]pyrimidin-2-yl]phenyl]-
N-Ethyl-N'-[4-[5,6,7,8-tetrahydro-4-[(3S)-3-methyl-4-morpholinyl]-7-(3-oxetanyl)pyrido[3,4-d]pyrimidin-2-yl]phenyl]urea USP/EP/BP
GDC-0349 N-Ethyl-N'-[4-[5,6,7,8-tetrahydro-4-[(3S)-3-methyl-4-morpholinyl]-7-(3-oxetanyl)pyrido[3,4-d]pyrimidin-2-yl]phenyl]urea | [EINECS(EC#)]
200-258-5 | [Molecular Formula]
C24H32N6O3 | [MDL Number]
MFCD22417087 | [MOL File]
1207360-89-1.mol | [Molecular Weight]
452.549 |
| Chemical Properties | Back Directory | [Boiling point ]
571.3±50.0 °C(Predicted) | [density ]
1.269 | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 30 mg/ml; DMSO: 30 mg/ml; DMSO:PBS (pH 7.2) (1:9): 0.1 mg/ml; Ethanol: 10 mg/ml | [form ]
Powder | [pka]
13.87±0.46(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
N-Ethyl-N'-[4-[5,6,7,8-tetrahydro-4-[(3S)-3-methyl-4-morpholinyl]-7-(3-oxetanyl)pyrido[3,4-d]pyrimidin-2-yl]phenyl]urea is a potent and selective mTOR inhibitor with dose-dependent efficacy in mouse x
enograft cancer models. | [in vivo]
When dosed orally once daily in athymic mice in a MCF7-neo/Her2 tumor xenograft model (PI3K mutation), GDC-0349 (Compound 8h) inhibits tumor growth in a dose-dependent manner, achieving stasis (99% TGI) at the maximum tolerated dose. Body weight change is less than 10% up to the highest dose. GDC-0349 is also efficacious in other xenograft models, including PC3 (PTEN null) and 786-0 (VHL mutant). Similar levels of tumor growth inhibition are achieved when GDC-0349 is administered once every three days at higher doses compared to once every day. GDC-0349 has ~10-fold reduced free plasma clearance in both mice (100 mL/min/kg) and rats (171 mL/min/kg in rat)[1]. | [target]
mTOR | [IC 50]
mTOR: 3.8 nM (Ki); mTORC1; mTORC2; Autophagy | [storage]
Store at -20°C |
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